Bioorganic & medicinal chemistry letters, 2001-04, Vol.11 (7), p.865-869
2001
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Details
- Autor(en) / Beteiligte
- Titel
- 2-Arylindole-3-acetamides: FPP-Competitive inhibitors of farnesyl protein transferase
- Ist Teil von
- Bioorganic & medicinal chemistry letters, 2001-04, Vol.11 (7), p.865-869
- Ort / Verlag
- Oxford: Elsevier Ltd
- Erscheinungsjahr
- 2001
- Quelle
- Elsevier Journal Backfiles on ScienceDirect (DFG Nationallizenzen)
- Beschreibungen/Notizen
- A series of 2-arylindole-3-acetamide farnesyl protein transferase inhibitors has been identified. The compounds inhibit the enzyme in a farnesyl pyrophosphate-competitive manner and are selective for farnesyl protein transferase over the related enzyme geranylgeranyltransferase-I. A representative member of this series of inhibitors demonstrates equal effectiveness against HDJ-2 and K-Ras farnesylation in a cell-based assay when geranylgeranylation is suppressed. Graphic
- Sprache
- Englisch
- Identifikatoren
- ISSN: 0960-894XeISSN: 1464-3405DOI: 10.1016/S0960-894X(01)00061-0Titel-ID: cdi_proquest_miscellaneous_77032267
- Format
- –
- Schlagworte
- Alkyl and Aryl Transferases - antagonists & inhibitors, Alkyl and Aryl Transferases - metabolism, Antineoplastic agents, Biological and medical sciences, Carrier Proteins - metabolism, Enzyme Inhibitors - chemical synthesis, Enzyme Inhibitors - metabolism, Enzyme Inhibitors - pharmacology, General aspects, Heat-Shock Proteins - metabolism, HSP40 Heat-Shock Proteins, Humans, Indoleacetic Acids - chemical synthesis, Indoleacetic Acids - metabolism, Indoleacetic Acids - pharmacology, Medical sciences, Pharmacology. Drug treatments, Protein Prenylation - drug effects, Protein Prenylation - physiology, ras Proteins - metabolism, Structure-Activity Relationship, Tumor Cells, Cultured